Tetrapyrrole compounds play vital roles in the life processes of animals and plants, such as respiration and photosynthesis, due to their functions in light energy capture and transmission, signal transduction, and binding and transport of oxygen, and their research originated from the study of heme and chlorophyll chemistry. The special structure of tetrapyrrole determines its various properties, which contribute to its antioxidant, anti-inflammatory, antitumoral, antibacterial, neuroprotective and other biological activities. Although many functions of tetrapyrrole compounds have been excavated and utilized, there is a lack of a complete system to summarize them. This review summarizes the biosynthesis, functional evolution, biomedical applications and optical applications of tetrapyrrole compounds based on existing research on tetrapyrrole compounds.